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Polycyclic heteroaryl substituted triazoles useful as Axl inhibitors
专利权人:
RIGEL PHARMACEUTICALS; INC.
发明人:
SINGH, RAJINDER,HECKRODT, THILO J.,HOLLAND, SACHA
申请号:
ES09790061
公开号:
ES2537480T3
申请日:
2009.07.02
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula (I): ** Formula ** in which: A is>; = C (H) - or>; = N-; R1 is -N (R2) R3, -N (R2) C (O) R3 or -N (R2) -R4-C (O) OR3; or R1 is an N-heterocyclyl optionally substituted with one or more substituents selected from the group consisting of halo and -R4-C (O) OR2; each R2 and R3 is hydrogen, alkyl, alkenyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl and optionally substituted heteroarylalkyl; and each R4 is independently selected from the group consisting of a direct bond and an optionally substituted linear or branched alkylene chain; as an isolated stereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof; with the proviso that the compound of formula (I) is not a compound selected from the group consisting of: 1 - ((6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-c] pyridazin -3-yl) -N3- (7- (pyrrolidin-1-yl) -6,7,8,9-tetrahydro-5Hbenzo [7] anulen-2-yl) -1H-1,2,4-triazole- 3,5-diamine; 1 - ((6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-c] pyridazin-3-yl) -N3- (7 - ((bicyclo [2, 2,1] heptan-2-yl) amino) -6,7,8,9-tetrahydro-5H-benzo [7] anulen-2-yl) -1H-1,2,4-triazol-3,5- diamine; 1 - ((6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-c] pyridazin-3-yl) -N3- (7 - ((bicyclo [2,2,1]) heptan-2-yl) (methyl) amino) -6,7,8,9-tetrahydro-5H-benzo [7] anulen-2-yl) -1H-1,2,4-triazol-3,5-diamine ; 1 - ((6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-c] pyridazin-3-yl) -N3 - ((7-piperidin-1-yl) -6.7 , 8,9-tetrahydro-5Hbenzo [7] anulen-2-yl) -1H-1,2,4-triazol-3,5-diamine; 1- ((6,7-dihydro-5H-benzo [6, 7] cyclohepta [1,2-c] pyridazin-3-yl) -N3 - ((7-azetidin-1-yl) -6,7,8,9-tetrahydro-5H-benzo [7] nullify 2- il) -1H-1,2,4-triazol-3,5-diamine; 1 - ((6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-c] piri dazin-3-yl) -N3 - ((7- (R) -pyrrolidin-1-yl) -6,7,8,9-tetrahydro-5Hbenzo [7] anulen-2-yl) -1H-1,2 , 4-triazol-3,5-diamine; and 1 - ((6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-c] pyridazin-3-yl) -N3
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